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This study aimed to observe the protective effect of momordicine I, a triterpenoid compound extracted from momordica charantia L., on isoproterenol (ISO)-induced hypertrophy in rat H9c2 cardiomyocytes and investigate its potential mechanism. Treatment with 10 μM ISO induced cardiomyocyte hypertrophy as evidenced by increased cell surface area and protein content as well as pronounced upregulation of fetal genes including atrial natriuretic peptide, β-myosin heavy chain, and α-skeletal actin; however, those responses were markedly attenuated by treatment with 12.5 μg/ml momordicine I. Transcriptome experiment results showed that there were 381 and 447 differentially expressed genes expressed in comparisons of model/control and momordicine I intervention/model, respectively. GO enrichment analysis suggested that the anti-cardiomyocyte hypertrophic effect of momordicine I may be mainly associated with the regulation of metabolic processes. Based on our transcriptome experiment results as well as literature reports, we selected glycerophospholipid metabolizing enzymes group VI phospholipase A 2 (PLA2G6) and diacylglycerol kinase ζ (DGK-ζ) as targets to further explore the potential mechanism through which momordicine I inhibited ISO-induced cardiomyocyte hypertrophy.Our results demonstrated that momordicine I inhibited ISO-induced upregulations of mRNA levels and protein expressions of PLA2G6 and DGK-ζ. Collectively, momordicine I alleviated ISO-induced cardiomyocyte hypertrophy, which may be related to its inhibition of the expression of glycerophospholipid metabolizing enzymes PLA2G6 and DGK-ζ.
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To explore the potential mechanism of frankincense volatile oil in the prevention and treatment of cardiac hypertrophy based on in vitro cell experiment and network pharmacology. METHODS: The anti-hypertrophic effect of frankincense volatile oil was investigated by isoproterenol induced H9c2 cardiomyocytes hypertrophy model. The active chemical components and targets of frankincense volatile oil and targets associated with cardiac hypertrophy were obtained by CNKI, Pubmed, Pubchem databases, etc. String database and Cytoscape 3.8.0 software were used to construct protein-protein interaction network (PPI) and a network of "drug-active component-key target-disease" of frankincense volatile oil in order to screen the key targets of frankincense volatile oil against cardiac hypertrophy. The fluorescent quantitative PCR experiments were performed to verify those key targets. Gene Ontology (GO) enrichment analysis and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway annotation analysis of key target genes were performed using David online analysis tool. RESULTS: In vitro cell experiments showed that frankincense volatile oil significantly inhibited the isoproterenol induced increases in cardiomyocytes surface area and protein synthesis, and upregulations of ANP and β-MHC mRNA. A total of 87 active components and 36 ingredient-disease targets of frankincense volatile oil were screened. Network analysis showed that ESR1, NOS3, PTGS2, TNF, MAPK14, and PPARG were key targets. Fluorescence quantitative PCR experiments results indicated that frankincense volatile oil inhibited isoproterenol induced upregulations of ESR1, PTGS2, TNF, and MAPK14 mRNA levels, and downregulations of NOS3, PPARG mRNA levels, respectively. In addition, the GO functional enrichment analysis showed that its biological pathways mainly included lipopolysaccharide-mediated signaling pathway, positive regulation of nitric oxide biosynthetic process, caveola, enzyme binding, etc. The KEGG pathway enrichment analysis included 22 KEGG pathways, which were closely related to VEGF signaling pathway, TNF signaling pathway, sphingolipid signaling pathway and others. CONCLUSION: The active components of frankincense volatile oil may regulate VEGF signaling pathway, TNF signaling pathway, Sphingolipid signaling pathway by acting on ESR1, NOS3, PTGS2, TNF, MAPK14 and PPARG targets, thereby affecting the regulation of lipopolysaccharide-mediated signaling pathway, positive regulation of nitric oxide biosynthetic process, caveola, and enzyme binding, and improving cardiac hypertrophy.
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AIM: To investigate the effect of oxypeucedanin (OPD) on doxorubicin resistance in human breast cancer MCF-7/DOX cells and its possible mechanism. METHODS: MCF-7/DOX cells were cultured in vitro, MTT assay was used to detect the effect of OPD on the survival of MCF-7/DOX cells, and the effect of OPD combined with different concentrations of doxorubicin on the proliferation of MCF-7/DOX cells were investigated. The effect of OPD combined with doxorubicin on the expression of genes including MDR1, MRP1, AGPAT2, CHKA, CEPT1, DGKA, PCYT1A, PLA2G15 in MCF-7/DOX cells was measured by qRT-PCR. The effect of OPD combined with doxorubicin on the protein expression of MDR1, MRP1, CHKA and CCTα in MCF-7/DOX cells was determined by Western blot. RESULTS: The IC
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OBJECTIVE:To observe the protective effect of the traditional Chinese medicine Yiqimingmu oral solution on photochemical damage of retina in rats. METHODS:SD rats were divided into four groups randomly:negative control group, model group, low dose Yiqimingmu oral solution group and high dose Yiqimingmu oral solution group. All the groups except the control one were continually exposed to Lux (1 900?106.9) green fluorescent light for 24 hours to establish retinal photochemical damage model. The low dose and high dose groups were administered intragastrically with Yiqimingmu oral solution (15mL?kg-1?d-1 and 30mL?kg-1?d-1) 7 days before light expose. Normal saline solution was administered intragastrically in control and model group. At 6 hours and 6, 14 days after light expose, the content of malandialdehyde (MDA) and activity of SOD in rats' retina were measured. The histopathologic changes were observed by transmission electron microscopy and light microscopy. RESULTS:At 6 and 14 days after light expose, the activity of SOD in Yiqimingmu solution high dose group were higher than in the model control group(P
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OBJECTIVE:To get to know the preoperative and postoperative medication of patients with cataract.METHODS:The preoperative and postoperative medication of 564 cases with cataract extraction in our hospital from September 2004 to October 2004 was analyzed statistically.RESULTS:Antibacterial eye gutta was mainly used before cataract extraction while compound eye gutta containing antiseptic drugs and glucocorticosteroid were chiefly used after cataract operation.CONCLUSION:The preoperative and postoperative medication for patients with cataract in our hospital was reasonable.
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OBJECTIVE:To provide recommendation for the clinic on the optimal application concentration of potassium permanganate collyria.METHODS:3different concentrations of potassium permanganate collyria were prepared,the local ir-ritation of2of which on eyes of115conjunctivitis cases receiving conjunctival sac irrigation and the effects of the3different concentrations of potassium permanganate collyria on the comfort degree,corneal epithelium and bacterial colonies before and after eye irrigation of18pairs of oculus normalis receiving conjunctival sac irrigation were observed.RESULTS:Of the total115conjunctivitis cases,98(about85%)complained to have severe irritation;8cases(about7%)felt unbearable because of the strong irritation.Degree of comfort decreased with the elevation of concentration of collyria,while failed to have any effect on corneal epithelium and the numbers of bacterial colonies before and after irrigation.CONCLUSION:The recommended concentration of100ml∶1.5mg of potassium permanganate collyria for the irrigation of conjunctival sac in the clinic.
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OBJECTIVE:To establish the method for the content determination of Ciclosporin ophthalmic emulsion and to probe into its stability.METHODS:HPLC method was used to determine the content of ciclosporin.The separation was performed on Eclipse XDB-C8 column.The mobile phase consisted of acetonitrile-methanol-water(67.5 :5 :27.5) with the flow rate of 0.8 mL?min-1.The detection wavelength was set at 210 nm and column temperature was 55 ℃.Its stability was studied by classic isothermal accelerated test and highlight struck test.RESULTS:The linear range of ciclosporin was 5～60 mg?L-1(r=0.999 9) with average recovery of 100.39%(RSD=1.15%).The preparation was stable under heat and light,and its shelf life at 25 ℃ was predicted about 6.88 years.CONCLUSIONS:The method is accurate and feasible for the content determination of Ciclosporin ophthalmic emulsion.The preparation can be stored at room temperature.
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OBJECTIVE: To investigate the stimulation effect of several bacterial inhibitors of eye drops on eyes.METHODS: Stimulation effect of several bacterial inhibitors on rabbits eyes were observed with the contrast on the same body.The scores were counted according to the score standard of eyes stimulation response in order to evaluate the stimulation effect of bacterial inhibitors.RESULTS: After giving single dose of inhibitors,the average scores of stimulation reaction induced by 0.002% thiomersal,0.01% benzalkonium chloride,0.01% benzalkonium bromide,0.01% chlorhexidin acetas,0.5% chlorobutanol,0.03% ethylparaben,2% boric acid were 0.20,0.32,0.36,0.60,1.20,3.88,6.32,mild stimulation reaction was induced by 2% boric acid and 0.03% ethylparaben and others inhibitors caused no stimulation response.After giving multiple doses of inhibitors,the average scores of above inhibitors were 0.49,0.79,0.84,3.83,3.91,6.51,10.84,the medium stimulation reaction was induced by 2% boric acid,mild stimulation reaction were induced by 0.03% ethylparaben,0.01% chlorhexidin acetas and 0.5% chlorobutanol;0.002% thiomersal,0.01% benzalkonium chloride,0.01% benzalkonium bromide caused no stimulation reaction.CONCLUSION: The best inhibitors of eye drops are thiomersal,benzalkonium chloride,benzalkonium bromide,followed by chlorhexidin acetas,ethylparaben,chlorobutanol.
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To find out the patterns and trend of clinical use of antihypertensive agents to provide a guidance for rational use of drugs, the antihypertensive drugs used in our hospital during 1995-1999 period was investigated in respect to the sum of consumption cost, drugs used and DDDs. Our results showed that the DDDs and the consumption cost for antihypertensive drugs have increased gradually for recent 5 years. The order of DDDs of drugs was as follows: calcium antagonists, adrenergic blocking drugs, ACE inhibitors, the drugs affecting sympathetic transmitters and peripheral vasodilators. The order of sum of money was as follows: ACE inhibitors, calcium antagonists and calcium antagonists respectively. It is concluded that a diverse array of anthhypertensive agents were available and widely used clinically and attention should be paid to the rational use of the drugs.
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OBJECTIVE:To study the effects of diltiazem on the blood concentration and the renal toxicity of cyclosporin A(CsA) in patients with renal transplantation.METHODS: 25 patients with renal transplantation were divided into two groups,the therapeutic group were treated with diltiazem plus CsA and control group CsA alone and the valley blood concentration of CsA was detected by FPIA assay.RESULTS:The dosage of CsA in therapeutic group was less than that in control group significantly,the levels of UA,Scr and BUN in patients were decreased by diltiazem.CONCLUSION:The diltiazem therapy can decrease the dosage and toxic effect of CsA,then save the patient's medical costs.
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OBJECTIVE:To observe the stability of phacolin eye drops.METHODS:The content and the stability of phacolin eye drops were determined by ultraviolet spectrophotometry and the initial average rate method respectively.RESULTS:The activation energy for pyrolytic reaction of phcolin eye drops was25.681kcal/mol,the shelflife of phacolin eye drops at room temperature(25℃)and10℃were88and878days respectively.CONCLUSION:The determination of the stability of phacolin eye drops with initial average rate method is useful and simple.